[EN] 4-AMINOQUINOLINE COMPOUNDS FOR THE TREATMENT OF ANGIOGENESIS<br/>[FR] COMPOSÉS DE 4-AMINOQUINOLINE POUR LE TRAITEMENT DE L'ANGIOGENÈSE
申请人:SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INST
公开号:WO2019173482A1
公开(公告)日:2019-09-12
Described herein is the use of 4-aminoquinoline compounds as inhibitors of angiogenesis, such as retinal pathological angiogensis. Also described herein are compositions and formulations comprising such compounds for the use in treatment of pathological angiogenesis.
Lewis Acid-Catalyzed Generation of CC and CN Bonds on π-Deficient Heterocyclic Substrates
作者:Matteo Staderini、Maria Laura Bolognesi、J. Carlos Menéndez
DOI:10.1002/adsc.201400674
日期:2015.1.12
to the efficient and completely regioselective generation of aromatic CC and CNbonds. The method is simple, rapid, general and inexpensive, and can be performed without the use of dried solvents. Most of the synthetized compounds are new and in many cases the work‐up required only filtration. Furthermore, this is the first example of the use of a Lewis acid as a catalyst for heteroarylation, vinylation
A series of tailor-made molecules, 1 and 4-7, have been prepared to recognize and cleave DNA at apurinic sites. These molecules incorporate in their structure different units designed for specific functions: (1) an intercalator for DNA binding, (2) a nucleic base for abasic site recognition, and (3) a linker endowed with both a binding function and a cleavage function (Scheme II). The constituent units were varied successively in the series of molecules to get insight into their mode of action and prepare more active compounds. H-1 NMR spectroscopy reveals the absence of intramolecular ring-ring stacking interactions in water between the base and the intercalator in all molecules 1 and 4-7. All bind to calf thymus DNA with binding constants ranging from 10(4) to 10(6) M-1. Their nuclease activity was estimated by measuring their ability to induce single strand breaks in depurinated pBR 322 plasmid DNA. The most efficient molecule, 5, exhibits high recognition selectivity and cleavage efficiency: at nanomolar concentrations, 5 recognizes and cleaves the abasic lesion present in a DNA molecule containing an average of 1.8 apurinic sites in its 4 362 base pairs sequence. Molecule 5 exhibits higher cleaving efficiency than the reported tripeptide Lys-Trp-Lys: 10(-8) M concentrations of the former (5) lead to cleavage ratios comparable to those observed for the latter used as 10(-3) M concentration. This enzyme mimic 5 can be used advantageously as a substitute to the natural nuclease for in vitro cleavage of depurinated DNA.
Ganapathi; Shah, Proceedings - Indian Academy of Sciences, Section A, 1951, # 34, p. 178,180
作者:Ganapathi、Shah
DOI:——
日期:——
The Role of Phenol in the Reaction of 4,7-Dichloroquinoline with Novol Diamine